Pyridine derivatives possessing hypoglycemic and analgesic activity

Slyusarenko, E. I.; Gorodetskova, N. P.; Pesotskaya, G. V.; Levchenko, E. S.; Mogilevich, S. E.; Luk'yanchuk, V. D.

doi:10.1007/bf00764439

Cited by 5 publications

(4 citation statements)

References 2 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…For the most safe and versatile therapeutic solutions, we diverged into the plethora of naturally occurring medicinal compounds, specifically, nitrogen containing heterocyclic rings. Piperidine, pyridine and pyrimidine derivatives have been known to inhibit carbohydrate digesting enzymes, in addition to their anti-inflammatory, antibacterial and anticancer potencies [13][14][15][16][17][18][19][20].…”

Section: Introductionmentioning

confidence: 99%

Structural elucidation, molecular docking, α-amylase and α-glucosidase inhibition studies of 5-amino-nicotinic acid derivatives

et al. 2020

View full text Add to dashboard Cite

In this study, 5-amino-nicotinic acid derivatives (1-13) have been designed and synthesized to evaluate their inhibitory potential against α-amylase and α-glucosidase enzymes. The synthesized compounds (1-13) exhibited promising α-amylase and α-glucosidase activities. IC 50 values for α-amylase activity ranged between 12.17 ± 0.14 to 37.33 ± 0.02 µg/mL ± SEM while for α-glucosidase activity the IC 50 values were ranged between 12.01 ± 0.09 to 38.01 ± 0.12 µg/mL ± SEM. In particular, compounds 2 and 4-8 demonstrated significant inhibitory activities against α-amylase and α-glucosidase and the inhibitory potential of these compounds was comparable to the standard acarbose (10.98 ± 0.03 and 10.79 ± 0.17 µg/mL ± SEM, respectively). In addition, the impact of substituent on the inhibitory potential of these compounds was assessed to establish structure activity relationships. Studies in molecular simulations were conducted to better comprehend the binding properties of the compounds. All the synthesized compounds were extensively characterized with modern spectroscopic methods including 1 H-NMR, 13 C-NMR, FTIR, HR-MS and elemental analysis.

show abstract

Section: Introductionmentioning

confidence: 99%

Structural elucidation, molecular docking, α-amylase and α-glucosidase inhibition studies of 5-amino-nicotinic acid derivatives

et al. 2020

View full text Add to dashboard Cite

show abstract

“…This effect is most evident at neutral pH, where 1-15 N-MNAM was found to preserve 1-15 N polarization pH, unlike 1-15 N-NAM. 1-15 N-MNAM can be synthesized from 1-15 N-NAM (69)(70)(71). Synthesis and detailed analysis of 1-15 N-MNAM hyperpolarization will be the subject of our future work.…”

Section: Hyperpolarization Of Na Mnam and Nrmentioning

confidence: 99%

Nitrogen-15 dynamic nuclear polarization of nicotinamide derivatives in biocompatible solutions

Peters,

Brahms,

Janicaud

et al. 2023

Sci. Adv.

View full text Add to dashboard Cite

Dissolution dynamic nuclear polarization (dDNP) increases the sensitivity of magnetic resonance imaging by more than 10,000 times, enabling in vivo metabolic imaging to be performed noninvasively in real time. Here, we are developing a group of dDNP polarized tracers based on nicotinamide (NAM). We synthesized 1- 15 N-NAM and 1- 15 N nicotinic acid and hyperpolarized them with dDNP, reaching (13.0 ± 1.9)% 15 N polarization. We found that the lifetime of hyperpolarized 1- 15 N-NAM is strongly field- and pH-dependent, with T 1 being as long as 41 s at a pH of 12 and 1 T while as short as a few seconds at neutral pH and fields below 1 T. The remarkably short 1- 15 N lifetime at low magnetic fields and neutral pH drove us to establish a unique pH neutralization procedure. Using 15 N dDNP and an inexpensive rodent imaging probe designed in-house, we acquired a 15 N MRI of 1- 15 N-NAM (previously hyperpolarized for more than an hour) in less than 1 s.

show abstract

“…Our research group has been working on multifunctional amino derivatives synthesis ( Nawaz et al, 2020 , Rahim etal., 2020, Taha etal., 2020, Gollapalli at al., 2018, Taha et al, 2018 , Ibrahim et al, 2020 ) with antidiabetic and cytotoxic activity ( Qureshi et al, 2020 , Nawaz et al, 2022 ), and for this research we synthesized pyrimidine derivatives. Pyrmidine, a multi therapeutical nitrogen carrying heterocyclic ring, proven against carbohydrate digesting enzymes, bacteria and even cancer cell line ( Taha et al, 2017 , Slyusarenko et al, 1989 , Nawaz et al, 2016 , Soylem et al, 2017 , Altaf et al, 2015 , Krause et al, 2017 , Salar et al, 2017 ) and also many other therapeutic benefits, was selected as parent molecule, to be treated with a variety of functional moieties and the resulting compounds were characterized as per protocol.…”

Section: Introductionmentioning

confidence: 99%

Microwave assisted synthesis of 2-amino-4-chloro-pyrimidine derivatives: Anticancer and computational study on potential inhibitory action against COVID-19

Qureshi

Nawaz

Hisaindee

et al. 2022

Arabian Journal of Chemistry

View full text Add to dashboard Cite

Pyridine derivatives possessing hypoglycemic and analgesic activity

Cited by 5 publications

References 2 publications

Structural elucidation, molecular docking, α-amylase and α-glucosidase inhibition studies of 5-amino-nicotinic acid derivatives

Structural elucidation, molecular docking, α-amylase and α-glucosidase inhibition studies of 5-amino-nicotinic acid derivatives

Nitrogen-15 dynamic nuclear polarization of nicotinamide derivatives in biocompatible solutions

Microwave assisted synthesis of 2-amino-4-chloro-pyrimidine derivatives: Anticancer and computational study on potential inhibitory action against COVID-19

Contact Info

Product

Resources

About